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含5-氟尿嘧啶短肽的合成及其抗肿瘤活性研究
Synthesis and Antitumor Activity of Dipeptyl 5-Fluorouracil-propyl (butyl) Ester Derivatives
【摘要】 <正> 肿瘤细胞与正常细胞在酶系上存在差别,利用这些差别,chakravarty等设计并合成缬-亮-赖三肽与苯二胺氮芥等抗肿瘤原药结合的抗肿瘤短肽药物,它们的抗肿瘤选择性比苯二胺氮芥等抗肿瘤原药提高5~7倍。我们在前文中报道了5-氟尿嘧啶乙酰(丙酰)二肽和三肽的合成及抗动物肿瘤试验,初步结果表
【Abstract】 Twenty new dipeptyl 5-fluorouracil-propyl and butyl ester hydrochlorides were prepared from 5-fluorouracil-propyl esters or 5-fluorouracil-butyl esters of amino acids with N-protected amino acid anhydrides. The antitumor activity of five of them were tested agai- nst Ehrlich Ascites Carcinoma in mice, HC1·Phe-Gly-O(CH2)35-fluorouracil and HC1·Val- Leu-O(CH2)35-fluorouracil showed an inhibition ratio of 89.4% and 86.8%, respectively.
【关键词】 dipeptide;
fluorouracil;
antitumor activity;
【Key words】 dipeptide; fluorouracil; antitumor activity;
【Key words】 dipeptide; fluorouracil; antitumor activity;
【基金】 国家教委博士点基金资助课题
- 【文献出处】 有机化学 ,Chinese Journal of Organic cHEMISTRY , 编辑部邮箱 ,1989年03期
- 【被引频次】3
- 【下载频次】122